THERMOSENSITIVE GELS CONTAINING CARBAMAZEPINE MICROSPHERES FOR INTRANASAL BRAIN TARGETING
Panchaxari Mallappa Dandagi, Rohit Sharma*, Anand Panchakshari Gadad,
Journal Title:World Journal of Pharmaceutical Research
Context: Carbamazepine, derived from tricyclic antidepressant drugs
is one of the most widely used antiepileptic drugs. It is characterized
by a considerable hepatic first-pass effect owing to the enzymatic autoinduction of its own metabolism. Objective: The objective of the present investigation was to prepare thermo-sensitive gels containing
Carbamazepine microspheres for intranasal brain targeting to prolong
the drug release and enhance the bioavailability. Materials and Methods: Carbamazepine loaded chitosan microspheres were prepared
by emulsion cross-linking method by varying the drug: polymer ratio and evaluated. Microsphere embedded gel was prepared using Pluronic
F127 and Pluronic F68 using the optimized microsphere formulation and evaluated for in vitro permeation and ex vivo permeation. Results: Microsphere
formulation containing drug and polymer in the ratio 1:4 was fou nd to be optimized. 17% PF-127 and 1% PF-68 were found to be promising gel vehicles. The microspheres in the viscous media showed a prolonged release, in comparison to the microspheres alone.
Histopathological studies proved that the optimized formulation does not produce any toxic
effect on the microscopic structure of nasal mucosa during ex vivo permeation studies. Conclusion: Formulated thermo-sensitive gel can prove to be a promising formulation for the
safe and effective intranasal delivery and subsequent brain targeting of Carbamazepine.